| People | Locations | Statistics |
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| Naji, M. |
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| Motta, Antonella |
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| Aletan, Dirar |
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| Mohamed, Tarek |
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| Ertürk, Emre |
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| Taccardi, Nicola |
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| Kononenko, Denys |
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| Petrov, R. H. | Madrid |
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| Alshaaer, Mazen | Brussels |
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| Bih, L. |
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| Casati, R. |
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| Muller, Hermance |
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| Kočí, Jan | Prague |
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| Šuljagić, Marija |
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| Kalteremidou, Kalliopi-Artemi | Brussels |
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| Azam, Siraj |
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| Ospanova, Alyiya |
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| Blanpain, Bart |
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| Ali, M. A. |
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| Popa, V. |
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| Rančić, M. |
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| Ollier, Nadège |
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| Azevedo, Nuno Monteiro |
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| Landes, Michael |
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| Rignanese, Gian-Marco |
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Grohganz, Holger
University of Copenhagen
in Cooperation with on an Cooperation-Score of 37%
Topics
Publications (43/43 displayed)
- 2024Molecular interactions of hydrated co-amorphous systems of prilocaine and lidocainecitations
- 2024Anti-plasticizing effect of water on prilocaine and lidocainecitations
- 2024Influence of water and trehalose on α- and β-relaxation of freeze-dried lysozyme formulationscitations
- 2023Thermal investigation on hydrated co-amorphous systems of nicotinamide and prilocainecitations
- 2023Considerations on the Kinetic Processes in the Preparation of Ternary Co-Amorphous Systems by Millingcitations
- 2022Effects of polymer addition on the non-strongly interacting binary co-amorphous system carvedilol-tryptophancitations
- 2022Impact of Molecular Surface Diffusion on the Physical Stability of Co-Amorphous Systemscitations
- 2021The influence of moisture on the storage stability of co-amorphous systemscitations
- 2021Comparison of co-former performance in co-amorphous formulationscitations
- 2020Determination of the Optimal Molar Ratio in Amino Acid-Based Coamorphous Systemscitations
- 2020Preparation of Co-Amorphous Systems by Freeze-Dryingcitations
- 2019Process Optimization and Upscaling of Spray-Dried Drug-Amino acid Co-Amorphous Formulationscitations
- 2019Exploring the chemical space for freeze-drying excipientscitations
- 2019Influence of Glass Forming Ability on the Physical Stability of Supersaturated Amorphous Solid Dispersionscitations
- 2019In situ co-amorphisation in coated tablets – The combination of carvedilol with aspartic acid during immersion in an acidic mediumcitations
- 2019Co-former selection for co-amorphous drug-amino acid formulationscitations
- 2018Influence of PVP molecular weight on the microwave assisted in situ amorphization of indomethacincitations
- 2018The Role of Glass Transition Temperatures in Coamorphous Drug-Amino Acid Formulationscitations
- 2018Glass-Transition Temperature of the β-Relaxation as the Major Predictive Parameter for Recrystallization of Neat Amorphous Drugscitations
- 2018In vitro and in vivo comparison between crystalline and co-amorphous salts of naproxen-argininecitations
- 2018The use of molecular descriptors in the development of co-amorphous formulationscitations
- 2018Glass-Transition Temperature of the β-Relaxation as the Major Predictive Parameter for Recrystallization of Neat Amorphous Drugs.
- 2018The Influence of Polymers on the Supersaturation Potential of Poor and Good Glass Formerscitations
- 2017Probing Pharmaceutical Mixtures during Milling:citations
- 2017Amorphization within the tabletcitations
- 2017Influence of preparation pathway on the glass forming abilitycitations
- 2017Performance comparison between crystalline and co-amorphous salts of indomethacin-lysinecitations
- 2017Correlation between calculated molecular descriptors of excipient amino acids and experimentally observed thermal stability of lysozymecitations
- 2016Influence of variation in molar ratio on co-amorphous drug-amino acid systemscitations
- 2016Glass forming ability of amorphous drugs investigated by continuous cooling- and isothermal transformationcitations
- 2016Development of a screening method for co-amorphous formulations of drugs and amino acidscitations
- 2016INFLUENCE OF THE COOLING RATE AND THE BLEND RATIO ON THE PHYSICAL STABILTIY OF CO-AMORPHOUS NAPROXEN/INDOMETHACINcitations
- 2016Glass solution formation in water - In situ amorphization of naproxen and ibuprofen with Eudragit® E POcitations
- 2016Investigation of physical properties and stability of indomethacin-cimetidine and naproxen-cimetidine co-amorphous systems prepared by quench cooling, coprecipitation and ball millingcitations
- 2016Properties of the Sodium Naproxen-Lactose-Tetrahydrate Co-Crystal upon Processing and Storagecitations
- 2015Formation mechanism of coamorphous drug−amino acid mixturescitations
- 2015Characterization of Amorphous and Co-Amorphous Simvastatin Formulations Prepared by Spray Dryingcitations
- 2015Well-plate freeze-dryingcitations
- 2015Solid-state properties and dissolution behaviour of tablets containing co-amorphous indomethacin-argininecitations
- 2014Near-Infrared Imaging for High-Throughput Screening of Moisture-Induced Changes in Freeze-Dried Formulationscitations
- 2013Amino acids as co-amorphous stabilizers for poorly water soluble drugs--Part 1citations
- 2013In situ amorphisation of indomethacin with Eudragit® E during dissolutioncitations
- 2011Coamorphous drug systems: enhanced physical stability and dissolution rate of indomethacin and naproxencitations
Places of action
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article
Amino acids as co-amorphous stabilizers for poorly water soluble drugs--Part 1
Abstract
<p>Poor aqueous solubility of an active pharmaceutical ingredient (API) is one of the most pressing problems in pharmaceutical research and development because up to 90% of new API candidates under development are poorly water soluble. These drugs usually have a low and variable oral bioavailability, and therefore an unsatisfactory therapeutic effect. One of the most promising approaches to increase dissolution rate and solubility of these drugs is the conversion of a crystalline form of the drug into its respective amorphous form, usually by incorporation into hydrophilic polymers, forming glass solutions. However, this strategy only led to a small number of marketed products usually because of inadequate physical stability of the drug (crystallization). In this study, we investigated a fundamentally different approach to stabilize the amorphous form of drugs, namely the use of amino acids as small molecular weight excipients that form specific molecular interactions with the drug resulting in co-amorphous forms. The two poorly water soluble drugs carbamazepine and indomethacin were combined with amino acids from the binding sites of the biological receptors of these drugs. Mixtures of drug and the amino acids arginine, phenylalanine, tryptophan and tyrosine were prepared by vibrational ball milling. Solid-state characterization with X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) revealed that the various blends could be prepared as homogeneous, single phase co-amorphous formulations indicated by the appearance of an amorphous halo in the XRPD diffractograms and a single glass transition temperature (Tg) in the DSC measurements. In addition, the Tgs of the co-amorphous mixtures were significantly increased over those of the individual drugs. The drugs remained chemically stable during the milling process and the co-amorphous formulations were generally physically stable over at least 6 months at 40 °C under dry conditions. The dissolution rate of all co-amorphous drug-amino acid mixtures was significantly increased over that of the respective crystalline and amorphous pure drugs. Amino acids thus appear as promising excipients to solve challenges connected with the stability and dissolution of amorphous drugs.</p>